Claims
- 1. A compound of general formula (I):
- 2. A compound according to claim 1 in which R1 represents C1-4 alkyl and R2 represents optionally substituted phenyl or optionally substituted phenylC1-4 alkyl, wherein the optional substituent on the phenyl ring is selected from acyl, acylamino, alkoxy, alkoxycarbonyl, alkylenedioxy, alkylsulphinyl, alkylsulphonyl, alkylthio, aroyl, aroylamino, aryl, arylalkyloxy, arylalkyloxycarbonyl, arylalkylthio, aryloxy, aryloxycarbonyl, arylsulphinyl, arylsulphonyl, arylthio, carboxy, cyano, halo, heteroaroyl, heteroaryl, heteroarylalkyloxy, heteroaroylamino, heteroaryloxy, hydroxy, nitro, trifluoromethyl, Y3Y4N—, Y3Y4NCO—, Y3Y4NSO2—, Y3Y4N—C2-6alkylene-Z— [where Z is O, NR4 or S(O)n], alkylC(═O)—Y3N—, alkylSO2—Y3N— or alkyl optionally substituted with aryl, heteroaryl, hydroxy, or Y3Y4N—.
- 3. A compound according to claim 1 in which R1 and R2 together with the nitrogen atom to which they are attached form a bicyclic ring system consisting of a cyclic amine containing a 5-7 membered monocyclic cycloalkyl group wherein one of the ring carbon atoms is replaced by a nitrogen atom which is fused via ring carbon atoms to an aryl ring.
- 4. A compound according to claim 3 in which the fused aryl ring is optionally substituted phenyl.
- 5. A compound according to claim 1 in which R1 and R2 together with the nitrogen atom to which they are attached form an indolinyl ring.
- 6. A compound according to claim 1 in which Ar1 represents aryldiyl.
- 7. A compound according to claim 6 in which Ar1 represents optionally substituted phenylene.
- 8. A compound according to claim 7 in which Ar1 represents p-phenylene or p-phenylene substituted by C1-4alkyl, C1-4alkoxy, C1-4alkylthio, C1-4alkylsulphinyl or C1-4alkylsulphonyl.
- 9. A compound according to claim 8 in which Ar1 represents p-phenylene or p-phenylene substituted by C1-4alkoxy.
- 10. A compound according to claim 8 in which the substituent is located in the 3 position
- 11. A compound according to claim 1 in which L1 represents a —R5—R6— linkage where R5 is a straight or branched C1-4alkylene chain and R6 represents —C(═O)—NH—.
- 12. A compound according to claim 11 in which L1 represents —CH2C(═O)—NH—
- 13. A compound according to claim 1 in which Ar2 represents optionally substituted p-phenylene.
- 14. A compound according to claim 13 in which Ar2 represents unsubstituted p-phenylene.
- 15. A compound according to claim 1 in which L2 represents a C1-4alkylene linkage optionally substituted by C1-4alkyl, aryl, heteroaryl, —Z2R8, —N(R7)—C(═O)—R8, —N(R7)—C(═O)—OR8, —N(R7)—SO2—R8, —NY1Y2, —[C(═O)—N(R9)—C(R4)(R10)]p—C(═O)—NY1Y2 or alkyl substituted by hydroxy, —OR3, —C(═O)—OR7 or —NY1Y2.
- 16. A compound according to claim 15 in which L2 represents ethylene optionally substituted by C1-4alkyl, aryl, heteroaryl, —Z2R8, —N(R7)—C(═O)—R8, —N(R7)—C(═O)—OR8, —N(R7)—SO2—R8, —NY1Y2, —[C(═O)—N(R9)—C(R4)(R10)]p—C(═O)—NY1Y2 or alkyl substituted by hydroxy, —OR3, —C(═O)—OR7 or —NY1Y2.
- 17. A compound according to claim 16 in which L2 is a group
- 17. A compound according to claim 16 in which L2 is a group
- 18. A compound according to claim 17 in which L2 is a group
- 19. A compound according to claim 18 in which R14 represents —N(R7)—C(═O)—R8, —N(R7)—C(═O)—OR8, —N(R7)—SO2—R8 or —NY1Y2.
- 20. A compound according to claim 18 in which R14 represents —N(R7)—C(═O)—R8.
- 21. A compound according to claim 1 in which Y is carboxy.
- 22. A compound according to claim 1 of formula (Ia):
- 23. A compound according to claim 1 of formula (Ib):
- 24. A compound according to claim 23 in which Ar4 is phenyl.
- 25. A pharmaceutical composition comprising an effective amount of a compound according to claim 1 or a corresponding N-oxide or prodrug, or a pharmaceutically acceptable salt or solvate of such a compound or an N-oxide prodrug thereof, in association with a pharmaceutically acceptable carrier or excipient.
- 26. A method for the treatment of a human or non-human animal patient suffering from, or subject to, a condition which can be ameliorated by the administration of an inhibitor of α4β1 mediated cell adhesion comprising administering to said patient an effective amount of a compound according to claim 1 or a corresponding N-oxide or prodrug, or a pharmaceutically acceptable salt or solvate of such a compound or an N-oxide or prodrug thereof.
- 27. A method for the treatment of a patient suffering from, or subject to, asthma comprising administering to said patient an effective amount of a compound according to claim 1 or a corresponding N-oxide or prodrug, or a pharmaceutically acceptable salt or solvate of such a compound or an N-oxide or prodrug thereof.
- 28. A method for the treatment of a patient suffering from, or subject to, an inflammatory disease comprising administering to said patient an effective amount of a compound according to claim 1 or a corresponding N-oxide or prodrug, or a pharmaceutically acceptable salt or solvate of such a compound or an N-oxide or prodrug thereof.
- 29. A method for the treatment of a human or non-human animal patient suffering from, or subject to, a condition which can be ameliorated by the administration of an inhibitor of α4β1 mediated cell adhesion comprising administering to said patient an effective amount of a composition according to claim 25.
- 30. A method for the treatment of a patient suffering from, or subject to, asthma comprising administering to said patient an effective amount of a composition according to claim 25.
- 31. A method for the treatment of a patient suffering from, or subject to, an inflammatory disease comprising administering to said patient an effective amount of a composition according to claim 25.
Priority Claims (3)
Number |
Date |
Country |
Kind |
9910417.6 |
May 1999 |
GB |
|
9910405.1 |
May 1999 |
GB |
|
9910396.2 |
May 1999 |
GB |
|
Parent Case Info
[0001] This application is a continuation of PCT/GB00/01734, filed May 5, 2000, which claims priority from GB Application Nos. 9910417.6, 9910405.1, and 9910396.2, all filed May 5, 1999, and U.S. Provisional Application Nos. 60/152,855, 60/152,861, and 60/152,860, all filed Sep. 8, 1999; all these applications incorporated herein by reference.
Provisional Applications (3)
|
Number |
Date |
Country |
|
60152855 |
Sep 1999 |
US |
|
60152861 |
Sep 1999 |
US |
|
60152860 |
Sep 1999 |
US |
Continuations (1)
|
Number |
Date |
Country |
Parent |
PCT/GB00/01734 |
May 2000 |
US |
Child |
10002747 |
Nov 2001 |
US |